cas 76003-29-7, 1-Boc-3-oxopiperazine | Articles data

Articles about 76003-29-7Total 51 be found

Article title
Article abstract
Author
Journal number and time
Download

Histamine H3 receptor antagonists with peptidomimetic (keto)piperazine structures to inhibit Aβ oligomerisation
Alzheime?s disease (AD) is the most prominent neurodegenerative disorder with high medical need. Protein-protein-interactions (PPI) interactions have a critical role in AD where β-amyloid structures (Aβ) build toxic oligomers. Design of disease modifying multi target directed ligand (MTDL) has been performed, which disable PPI on the one hand and on the other hand, act as procognitive antagonists at the histamine H3 receptor (H3R). The synthetized compounds are structurally based on peptidomimetic amino acid-like structures mainly as keto, diketo-, or acyl variations of a piperazine moiety connected to an H3R pharmacophore. Most of them showed low nanomolar affinities at H3R and some with promising affinity to Aβ-monomers. The structure–activity relationships (SAR) described offer new possibilities for MTDL with an optimized profile combining symptomatic and potential causal therapeutic approaches in AD.
Falkenstein, Markus,Reiner-Link, David,Zivkovic, Aleksandra,Gering, Ian,Willbold, Dieter,Stark, Holger
(2021/10/29)

Nitroimidazole compound as well as preparation method and application thereof
The invention discloses a novel nitroimidazole compound as well as a preparation method and application thereof. The nitroimidazole compound has a general formula (I) shown in the specification.
-
Paragraph 0274-0276; 0277-0278

(2021/02/10)

The hydrophobically-tagged MDM2-p53 interaction inhibitor Nutlin-3a-HT is more potent against tumor cells than Nutlin-3a
We present the first application of hydrophobic tagging to a non-covalent inhibitor of protein-protein interactions. Nutlin-3a-HT, created by fusing the hydrophobic tag HyT13 to the MDM2-p53 interaction inhibitor Nutlin-3a, prevented cellular accumulation of MDM2 upon p53 reactivation, and had a stronger effect on cell viability and the induction of apoptosis than Nutlin-3a.
Berg, Thorsten,Nietzold, Florian,Rubner, Stefan
supporting information
p. 14351 - 14354
(2019/12/02)

Tetrahydroisoquinoline amide compounds containing quaternary ammonium ion and pharmaceutical use thereof
The invention relates to tetrahydroisoquinoline amide compounds containing quaternary ammonium ion, a preparation method of the compounds, and a use of the compounds in the treatment or prevention ofthromboembolic diseases.
-
Paragraph 0383-0384

(2019/07/11)

PHENYL AMINO PIPERIDINE mTORC INHIBITORS AND USES THEREOF
The present invention provides compounds, compositions thereof, and methods of using the same.
-
Paragraph 0735; 0733

(2018/05/24)

Dimer ester micromolecule PROTACs for inducing MDM2 to self-degrade E3 ubiquitin ligase
The invention provides dimer ester micromolecule PROTACs for inducing MDM2 to self-degrade E3 ubiquitin ligase. The structure of the PROTACs is shown in the specification, wherein in a compound (I), L1 is C1-C30 linear or branched alkyl with or without a substituent group, and any carbon atom in L1 is optionally replaced by heteroatom; R1, R2, R3 and R4 are C1-C30 linear or branched alkyl with orwithout a substituent group, C1-C30 aryl with or a without substituent group, C1-C30 linear or branched alkylaryl with or without a substituent group or C1-C30 linear or branched aryl alkyl with or without a substituent group respectively and independently; X1, X2, X3 and X4 are halogen respectively and independently.
-
Paragraph 0133; 0135; 0136; 0168

(2018/10/19)

Dimer amide micromolecule PROTACs for inducing MDM2 to self-degrade E3 ubiquitin ligase
The invention provides dimer amide micromolecule PROTACs for inducing MDM2 to self-degrade E3 ubiquitin ligase. The structure of the PROTACs is shown in the specification, wherein in a compound (I), L1 is C1-C30 linear or branched alkyl with or without a substituent group, and any carbon atom in L1 is optionally replaced by heteroatom; R1, R2, R3 and R4 are C1-C30 linear or branched alkyl with orwithout a substituent group, C1-C30 aryl with or without a substituent group, C1-C30 linear or branched alkylaryl with or without a substituent group or C1-C30 linear or branched aryl alkyl with or without a substituent group respectively and independently; X1, X2, X3 and X4 are halogen respectively and independently.
-
Paragraph 0132; 0134; 0135

(2018/10/19)

Containing piperazinone quinazoline ketone PARP - 1/2 inhibitor and its preparation method, pharmaceutical composition and use thereof (by machine translation)
The invention discloses a new class of containing piperazinone quinazoline - 2, 4 (1 H, 3 H) - dione PARP - 1/2 inhibitor, and its preparation and pharmaceutical composition and use. Specifically, the invention relates to the general formula I shown containing of the piperazinone quinazoline - 2, 4 (1 H, 3 H) - dione derivatives and their pharmaceutically acceptable salt, and its preparation method, comprising one or more of the compounds of the composition, and the compounds in the preparation, the prevention and/or treatment with PARP - 1/2 of a disease associated with the use of the medicament. (by machine translation)
-
Paragraph 0147-0149

(2017/09/08)

METALLOENZYME INHIBITOR COMPOUNDS
The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
-
Page/Page column 148

(2017/07/31)

HEPATITIS B VIRAL ASSEMBLY EFFECTORS
Novel assembly effector compounds having a therapeutic effect against hepatitis B viral (HBV) infection are disclosed. Assembly effector molecules described herein can lead to defective viral assembly and also may affect other viral activities associated with chronic HBV infection. Also disclosed is a process to synthesize disclosed compounds, method of treatment of HBV by administration of disclosed compounds, and use of these compounds in the manufacture of medicaments against HBV.
-
Paragraph 00291

(2016/10/31)

Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth
A series of fluorene-based derivatives was synthesized and evaluated for inhibiting both InhA and Mycobacterium tuberculosis growth. These compounds were inspired by the previously reported Genz-10850 molecule, a good InhA inhibitor, but with a poor activity against M. tuberculosis growth. Structure-activity relationships were performed by introducing the following chemical modifications: 1) the piperazine ring; 2) the amide group; 3) the aryl moiety; and 4) the fluorene moiety. Among these new derivatives, one of them was more effective against both the InhA activity and mycobacterial growth, compared to the hit compound. Docking studies were also performed to rationalize activities of these derivatives. Furthermore, we showed for the first time that efflux pump inhibitors potentiated the efficacy of Genz-10850 (GEQ) derivatives against M. tuberculosis growth, demonstrating that these compounds could be substrates of some efflux pumps.
Chollet, Aurélien,Mori, Giorgia,Menendez, Christophe,Rodriguez, Frédéric,Fabing, Isabelle,Pasca, Maria Rosalia,Madacki, Jan,Korduláková, Jana,Constant, Patricia,Quémard, Anna?k,Bernardes-Génisson, Vania,Lherbet, Christian,Baltas, Michel
supporting information
p. 218 - 235
(2015/07/07)

MACROCYLIC PYRIMIDINE DERIVATIVES
The present invention relates to substituted macrocylic pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention have EF2K inhibitory activity and optionally also Vps34 inhibitory activity. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
-
Page/Page column 151

(2015/11/02)

PRMT5 INHIBITORS AND USES THEREOF
Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
-
Paragraph 00222

(2014/07/08)

BENZODIOXANES FOR INHIBITING LEUKOTRIENE PRODUCTION
The present invention relates to compounds of formula (I) wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
-
Page/Page column 94

(2013/09/26)

BENZODIOXANE INHIBITORS OF LEUKOTRIENE PRODUCTION FOR COMBINATION THERAPY
The present invention relates to a combination comprising compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein, and an additional active agent. The present invention also relates to pharmaceutical compositions comprising these combinations, and methods of using these combinations to treat various diseases and disorders.
-
Paragraph 0333

(2013/09/26)

PIPERAZINYL ANTIVIRAL AGENTS
Provided are compounds of Formula (I) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the Flaviviridae family of viruses such as hepatitis C virus (HCV).
-
Page/Page column 147-148

(2011/04/25)

FUSED HETEROCYCLIC COMPOUND
The present invention relates to a fused heterocyclic compound having the Formula 1, which is useful as a platelet aggregation inhibitor, a method for preparing the same, and a pharmaceutical composition for inhibiting platelet aggregation comprising the same.
-
Page/Page column 32

(2011/07/29)

Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors
Guided by structure-based design, we synthesized two novel series of potent inhibitors of BACE1 and generated extensive SAR around both the prime and non-prime side binding pockets. The key feature of both series is a cyclic amine motif specifically crafted to achieve interactions with both the flap and with the S2′ pocket.
Cumming,Le,Babu,Carroll,Chen,Favreau,Gaspari,Guo,Hobbs,Huang,Iserloh,Kennedy,Kuvelkar,Li,Lowrie,McHugh,Ozgur,Pan,Parker,Saionz,Stamford,Strickland,Tadesse,Voigt,Wang,Wu,Zhang,Zhang
experimental part
p. 3236 - 3241
(2009/04/07)

PYRAZOLE DERIVATIVES
A compound represented by formula (I): (wherein Ar1 represents a phenyl group which may have 1 to 3 substituents, or a non-substituted 5- or 6-membered aromatic heterocyclic group; Ar2 represents (i) a non-substituted phenyl group, (ii) a phenyl group which has been substituted by a lower alkyl group having 1 to 3 groups or atoms selected from among a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom, or (iii) a 5- or 6-membered nitrogen-containing aromatic heterocyclic group which has been substituted by 1 to 3 groups or atoms selected from among a lower alkyl group, a lower alkynyl group, a lower alkanoyl group, a carbamoyl group, a cyano group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom; and X represents a group represented by formula (II): (wherein the ring structure represents a 4- to 7-membered heterocyclic group which may have, in addition to the nitrogen atom shown in formula (II), one heteroatom selected from among nitrogen, oxygen, and sulfur, and which may be substituted by 1 to 4 groups or atoms selected from among a lower alkyl group, a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, an oxo group, a lower alkanoyl group, a lower alkylsulfonyl group, and a halogen atom)), a salt thereof, a solvate of the compound or the salt, and a drug.
-
Page/Page column 57

(2010/11/26)

PYRAZOLE DERIVATIVE
A compound represented by Formula (I): wherein Ar1 represents Formula (II): Ar2 represents a 5- or 6-membered aromatic heterocyclic group which may be substituted; and X represents Formula (III): a salt thereof, or a solvate of the compound or the salt. A potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.
-
Page/Page column 43; 72

(2010/11/27)

1,5-DIHETEROCYCLE-1H-TRIAZOLE DERIVATIVE
The present invention relates to a compound represented by Formula (I): wherein Ar1, Ar2, R1 and R2 each represent a substituent, a salt thereof, or a solvate of the compound or the salt, and to a medicine containing the same. According to the present invention, a potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.
-
Page/Page column 39

(2010/11/27)

HETEROCYCLIC SULFONAMIDE DERIVATIVES AS INHIBITORS OF FACTOR XA
The invention relates to compounds of formula (I), Chemical formula should be inserted here. Please see paper copy wherein R1 is hydrogen, C1-3alkyl, R5R6 aminoC1-5alkyl, where R5 and R6 are each independently selected from hydrogen and C1-3alkyl, or R5 and R6 may, together with the nitrogen to which they are attached, form a five- or six-membered heterocyclic ring, where said heterocyclic ring has 0 or 1 additional heteroatom; n is 1 or 2; each R2 are independently selected from hydrogen, oxo and C1-3alkyl, R3 is an indolyl, and R4 a hydrogen or a halogen; or a pharmaceutically acceptable salt thereof, said compounds possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the compounds, to their use, to pharmaceutical compositions comprising them, to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, and to combinations comprising them.
-
Page/Page column 27

(2010/11/25)

CYANOGUANIDINE-SUBSTITUTED PYRAZOLINES
The invention relates to the field of blood coagulation and, in particular, to the use of cyanoguanidine-substituted pyrazolines as medicaments, novel cyanoguanidine-substituted pyrazolines of formula (1) and to methods for the production thereof, in addition to the use thereof for producing medicaments for treating and/or for the prophylaxis of illnesses, in particular cardiovascular diseases, preferably thromboembolic diseases.
-
Page/Page column 37

(2008/06/13)

AZETIDINE-SUBSTITUTED PYRAZOLINES AS PAR-1 ANTAGONISTS
The invention relates to blood clotting, and especially to the use of azetidine-substituted pyrazolines as medicaments, novel azetidine-substituted pyrazolines, methods for the production thereof, and the use of the same for producing medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular diseases, preferably thromboembolic diseases.
-
Page/Page column 30

(2008/06/13)

SUBSTITUTED AMIDE BETA SECRETASE INHIBITORS
Disclosed are novel compounds of the formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula (I). Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula (I) and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula (I), HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
-
Page/Page column 37

(2010/10/19)

MACROCYCLIC BETA-SECRETASE INHIBITORS
Disclosed are novel compounds of the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula (I). Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula (I) and at least one compound selected from the group consisting of -secretase inhibitors other than those of formula (I), HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
-
Page/Page column 29

(2010/10/19)

FIVE-MEMBERED HETEROCYCLIC DERIVATIVE
The present invention relates to a compound represented by formula (I): a salt of the compound, or a solvate of the compound or the salt; a drug containing any of the compounds, the salts, and the solvates; a preventive and/or therapeutic agent for an ischemic disease containing any of the compounds, the salts, and the solvates; and a platelet coagulation inhibitor containing any of the compounds, the salts, and the solvates. The compound of the present invention is useful as a strong platelet coagulation inhibitor without inhibiting COX-1 or COX-2.
-
Page/Page column 47; 51-52

(2010/11/08)

PHOSPHONATE ANALOGS OF HIV INTEGRASE INHIBITOR COMPOUNDS
Novel HIV integrase inhibitor compounds having at least one phosphonate group, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.
-
Page/Page column 407

(2010/02/15)

CYCLIC AMINE BASE-1 INHIBITORS HAVING A HETEROCYCLIC SUBSTITUENT
Disclosed are novel compounds of the formula (I)or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is formula (I) X is -0-, -C(R14)2- or -N(R)-; Z is -C(R14)2- or -N(R)-; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, -CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, -OR35, -N(R24)(R25)or -SR35; R41 is alkyl, cycloalkyl, -S02(alkyl), -C(O)-alkyl, -C(O)-cycloalkyl or -alkyl-NH-C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula (I). Also disclosed are pharmaceutical compositions and methods of treatment comprising compounds of formula I in combination with other agents useful in treating cognitive or neurodegenerative diseases.
-
Page/Page column 59

(2008/06/13)

CYCLIC AMINE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT
Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R is-C(O)-N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer’s disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, and N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
-
Page/Page column 75-76

(2008/06/13)

PYRAZOLE DERIVATIVE
Not available
-
Page/Page column 63

(2008/06/13)

BIARYL PIPERAZINYL-PYRIDINE ANALOGUES
Biaryl piperazinyl -pyri dine analogues are provided, of the Formula (I): wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands, for receptor localization studies.
-
Page 78

(2008/06/13)

N-(3-amino-2-hydroxy-propyl) substd. alkylamidoalkanol compd.
Disclosed are compounds of the formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
-
Page/Page column 129-130

(2008/06/13)

PYRROLOPYRIMIDINE DERIVATIVE
A pyrrolo[3,2-d]pyrimidine derivative represented by the formula (I) or a pharamaceutically acceptable salt of the derivative. The derivative or salt is useful as a GSK-3 inhibitor.
-
Page 109

(2010/02/09)

PRE-ORGANIZED TRICYCLIC INTEGRASE INHIBITOR COMPOUNDS
Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. Formula (I). Al and A2 are moieties forming a five, six, or seven membered ring. L is a bond or a linker connecting a ring atom of Ar to N. X is O, S, or substituted nitrogen. Ar is aryl or heteroaryl. Q is N, +NR, or CR4. The aryl carbons may be independently substituted with substituents other than hydrogen. The compounds may include prodrug moieties covalently attached at any site.
-
Page 172;173

(2008/06/13)

N-(3-amino-2-hydroxy-propyl)substituted alkylamide compounds
Disclosed are compounds of the formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
-
(2008/06/13)

INHIBITORS OF PRENYL-PROTEIN TRANSFERASE
The present invention is directed to peptidomimetic piperazine-containing macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras
-
(2008/06/13)

Sulfonamide derivatives, processes for producing the same and utilization thereof
The present invention is to provide a compound or a salt thereof represented by the formula: wherein R1is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, X′ is an optionally substituted alkylene chain, Y is an optionally substituted divalent cyclic group, X is a chemical bond or an optionally substituted alkylene chain, and Z is (1) an optionally substituted amino group, (2) an optionally substituted imidoyl group or (3) an optionally substituted nitrogen-containing heterocyclic group, or a pro-drug thereof, which have activated coagulation factor X inhibitory activity and which are useful as anti-coagulants.
-
(2008/06/13)

ACYLHYDRAZINE DERIVATIVES, PROCESS FOR PREPARING THE SAME AND USE THEREOF
Novel acylhydrazine derivatives exhibiting an inhibitory activity against activated blood coagulation factor X, which are compounds of general formula (I)or salts thereof, wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; R1and R2are each hydrogen or optionally substituted hydrocarbyl, or alternatively R1and R2or the substituent of X1and R2may be united to form an optionally substituted ring; X1and X2are each free valency, optionally substituted alkylene, or optionally substituted imino; D is oxygen or sulfur; A is -N(R3)-Y- or -N=Y-, R3is hydrogen, optionally substituted hydrocarbyl, or acyl; Y is an optionally substituted chain hydrocarbon group or an optionally substituted cyclic group; and Z is (1) optionally substituted amino, (2) optionally substituted imidoyl, or (3) an optionally substituted nitrogenous heterocycle group.
-
Page 42

(2010/11/30)

N-acylsulfonamide apoptosis promoters
N-Benzoyl arylsulfonamides having the formula are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.
-
(2008/06/13)

N-Acylsulfonamide apoptosis promoters
N-Benzoyl arylsulfonamides having the formula Are BCL-X1 inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-X1 inhibiting compositions and methods of promoting apoptosis in a mammal.
-
(2008/06/13)

Inhibitors of prenyl-protein transferase
The present invention is directed to peptidomimetic macrocyclic compounds of the formula A: wherein W is a heterocycle, V is a heterocycle or aryl moiety and Z1is a suitably substituted aryl or heterocycle moiety. The instant compounds inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
-
(2008/06/13)

Fused imidazopyridine derivatives as antihyperlipidemic agents
A novel compound of the formula: wherein ring Q is an optionally substituted pyridine ring; One of R0, R1and R2is —Y0—Z0, and the other tow groups are a hydrogen, a halogen, an optionally substituted hydroxy group, a hydrocarbon group that may be an optionally substituted hydrocarbon group or an acyl group; Y0is a bond or an optionally substituted bivalent hydrocarbon group; Z0is a basic group which may be bonded via oxygen, nitrogen, —CO—, —CS—, —SO2N(R3)— (where R3is hydrogen or an optionally substituted hydrocarbon group), or S(O)n(wherein n is to 0, 1 or 2); .........is a single bond or a double bond, or a salt thereof, which has an excellent LDL receptor up-regulating, blood-lipids lowering, blood-sugar lowering and diabetic complication-ameliorating activity.
-
(2008/06/13)

Aminoheterocyclic derivatives as antithrombotic or anticoagulant
The invention concerns compounds of formula (I), wherein each of G1, G2 and G6 is CH or n; m is 1 or 2; R1 includes hydrogen, halogeno and (1-4C)alkyl; M1 is a group of formula: NR2 -L1 -T1 R3, in which R2 and R3 together form a (1-4C)alkylene group, L1 includes (1-4C)alkylene, and T1 is CH or N; A may be a direct link; M2 is a group of the formula: (T2 R4)r -L2 T3 R5 in which R is 0 or 1, each of T2 and T3 is CH or N, each of R4 and R5 is hydrogen or (1-4C)alkyl, or R4 and R5 together form a (1-4C)alkylene group, and L2 includes (1-4C)alkylene; M3 may be a direct link to X; X includes sulphonyl; and Q includes naphthyl and a heterocycle moiety; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use as antithrombotic or anticoagulant agents.
-
(2008/06/13)

BICYCLIC HETEROARYL-ALKYLENE-(HOMO)PIPERAZINONES AND THIONE ANALOGUES THEREOF, THEIR PREPARATION, AND THEIR USE OF AS SELECTIVE AGONISTS OF 5HT1-LIKE RECEPTORS
A class of piperazinones, homopiperazinones and thione analogues thereof, substituted at the 1-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, and linked at the 4-position via an alkylene spacer to a fused bicyclic heteroaromatic moiety, typically indolyl, are selective agonists of 5-HT. sub.1-like receptors, being potent agonists of the human 5-HT 1Dα receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT 1Dα receptor subtype relative to the 5-HT 1D. beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT 1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT 1D receptor agonists.
-
(2008/06/13)

Heterocyclic compouds
A compound of the general formula wherein: n is 0 or 1; M1 is an amino group; Q is an aromatic heterocyclic group containing a basic nitrogen atom; M2 is an imino group; L is a template group; and A is an acidic group, or an ester or amide derivative thereof, or a sulphonamide group; and pharmaceutically acceptable salts and pro-drugs thereof, for use in the treatment of a disease in which platelet aggregation mediated by the binding of adhesion molecules to GPIIb-IIIa is involved. Novel compounds are also disclosed.
-
(2008/06/13)

Cyclic amidine analogs as inhibitors of nitric oxide synthase
Disclosed herein are compounds of Formula I STR1 and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation. These disease and disorders include hypotension, septic shock, toxic shock syndrom, hemodialysis, IL-2 therapy such as in cancer patients, cachexia, immunosuppression such as in transplant therapy, autoimmune and/or inflammatory indications including sunburn or psoriasis and respiratory conditions such as bronchitis, asthma, and acure respiratory distress (ARDS), myocarditis, heart failure, atherosclerosis, arthritis, rheumatoid arthritis, chronic or inflammatory bowel disease, ulcerative colitis, Crohn's disease, systemic lupus erythematosis (SLE), ocular conditions such as ocular hypertension and uveitis, type 1 diabetes, insulin-dependent diabetes mellitus and cystic fibrosis. Compounds of Formula I are also usful in the treatment of hypoxia, hyperbaric oxygen convulsions and toxicity, dementia, Sydenham's chorea, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, mulitple sclerosis, Korsakoff's disease, imbecility related to cerebral vessel disorder, ischemic brain edema, sleeping disorders, schizophrenia, depression, PMS, anxiety, drug addiction, pain, migraine, immune complex disease, as immunosupressive agents and for preventing or reversing tolerance to opiates and diazepines.
-
(2008/06/13)

Heterocyclic derivatives
Compounds of formula I STR1 and metabolically labile esters and amides thereof, and pharmaceutically acceptable salts thereof, in which R13, M2, X1, Z1, Z1a, X2 and A1 have the meanings given in the specification. The compounds are useful as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa. Novel intermediates are also disclosed.
-
(2008/06/13)

Heterocyclic derivatives
Compounds of formula I STR1 and metabolically labile esters and amides thereof, and pharmaceutically acceptable salts thereof, in which R13, M2, X1, Z1, Z1a, X2 and A1 have the meanings given in the specification. The compounds are useful as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa. Intermediates are also disclosed.
-
(2008/06/13)

Enkaphalin derivatives
Novel analgesic and antipsychotic agents having the formula STR1 wherein Q is STR2 in which R1 is hydrogen, hydroxy or halogen and R4 is hydrogen or, R1 and R4 are both hydroxy; Z is hydrogen or straight chain lower alkyl having from 1 to 4 carbon atoms and X is methylene, carbonyl, hydroxymethylene, thio, sulfinyl or sulfonyl, or Z and X, taken together, are methylidenyl, with the proviso that when X is sulfonyl or sulfinyl, Z is other than hydrogen; R5 is hydrogen or halogen, and R2 is H, a straight or branched lower alkyl group having from 1 to 4 carbon atoms, the group STR3 or the group STR4 wherein R3 is hydroxy, amino, alkylamino or dialkylamino wherein the alkyl moiety is straight or branched and has from 1 to 4 carbon atoms, diastereomers, enantiomers and pharmaceutically acceptable salts thereof.
-
(2008/06/13)